PE20080888A1 - HETEROCYCLIC COMPOUNDS AS ACIL-TRANSFERASE INHIBITORS OF ACIL-CoA-DIACIL-GLYCEROL 1 (DGAT1) - Google Patents

HETEROCYCLIC COMPOUNDS AS ACIL-TRANSFERASE INHIBITORS OF ACIL-CoA-DIACIL-GLYCEROL 1 (DGAT1)

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Publication number
PE20080888A1
PE20080888A1 PE2007001396A PE2007001396A PE20080888A1 PE 20080888 A1 PE20080888 A1 PE 20080888A1 PE 2007001396 A PE2007001396 A PE 2007001396A PE 2007001396 A PE2007001396 A PE 2007001396A PE 20080888 A1 PE20080888 A1 PE 20080888A1
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PE
Peru
Prior art keywords
acil
halogen
diacil
dgat1
coa
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PE2007001396A
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Spanish (es)
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Moo Sung
Gary Mark Coppola
Taeyoung Yoon
Thomas A Gilmore
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Novartis Ag
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Publication of PE20080888A1 publication Critical patent/PE20080888A1/en

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
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    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/18—Benzimidazoles; Hydrogenated benzimidazoles with aryl radicals directly attached in position 2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/12—Antihypertensives
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C07D209/48—Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
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    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/56—Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D263/57—Aryl or substituted aryl radicals
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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  • Organic Chemistry (AREA)
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  • Diabetes (AREA)
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  • Cardiology (AREA)
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  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Indole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

SE REFIERE A COMPUESTOS DE FORMULA A-L1-B-C-D, EN DONDE A ES UN ALQUILO(C1-C20), ALCOXILO(C1-C20), CICLOALQUILO(C3-C12), ENTRE OTROS; L1 ES -(CH2)n-(CR4R4')p-(CH2)m-N(R3)-, -(CH2)n-(CR4R4')p-(CH2)m-N(R3)-C(S)-, -C(NH)-N(R3)-(CH2)n-(CR4R4')p-(CH2)m-, ENTRE OTROS, DONDE R3 ES H O ALQUILO INFERIOR(C1-C7); m, n Y p SON CADA UNO DE 0 A 2; R4 Y R4' SON CADA UNO H, HALOGENO, HIDROXILO, ALCOXILO INFERIOR(C1-C7), ENTRE OTROS; B ES UN COMPUESTO DE FORMULA (i), (ii), ENTRE OTROS, DONDE X1 Y X2' SON CADA UNO O, NH, S, ENTRE OTROS; X1', X2, X3 Y X4 SON CADA UNO N O CH; C ES UN COMPUESTO DE FORMULA (iii), ARILO(C6-C14), ENTRE OTROS, DONDE R1 ES H, CN, HALOGENO, CF3, ENTRE OTROS; R'1, R2 Y R'2 SON CADA UNO H, HALOGENO, CF3, ALQUILO INFERIOR(C1-C7), ENTRE OTROS; D ES H, HALOGENO, HIDROXILO, CN, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ETIL-ESTER DEL ACIDO [2-(2-CLORO-FENIL)-3H-BENZOIMIDAZOL-5-IL]-CARBAMICO, ETIL-ESTER DEL ACIDO [2-(4-METOXI-2-METIL-FENIL)-3H-BENZOIMIDAZOL-5-IL]-CARBAMICO, ETIL-ESTER DEL ACIDO [2-(2,6-DIMETIL-FENIL)-3H-BENZOIMIDAZOL-5-IL]-CARBAMICO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA ACIL-TRANSFERASA DE ACIL-CoA-DIACIL-GLICEROL 1 (DGAT1) SIENDO UTILES EN EL TRATAMIENTO DE TOLERANCIA DETERIORADA A LA GLUCOSA, DIABETES TIPO 2, OBESIDAD, ANOREXIA NERVIOSAREFERS TO COMPOUNDS OF FORMULA A-L1-B-C-D, WHERE A IS AN ALKYL (C1-C20), ALCOXYL (C1-C20), CYCLOALKYL (C3-C12), AMONG OTHERS; L1 ES - (CH2) n- (CR4R4 ') p- (CH2) mN (R3) -, - (CH2) n- (CR4R4') p- (CH2) mN (R3) -C (S) -, - C (NH) -N (R3) - (CH2) n- (CR4R4 ') p- (CH2) m-, AMONG OTHERS, WHERE R3 IS HO LOWER ALKYL (C1-C7); m, n AND p ARE EACH FROM 0 TO 2; R4 AND R4 'ARE EACH H, HALOGEN, HYDROXYL, LOWER ALCOXYL (C1-C7), AMONG OTHERS; B IS A COMPOUND OF FORMULA (i), (ii), AMONG OTHERS, WHERE X1 AND X2 'ARE EACH O, NH, S, AMONG OTHERS; X1 ', X2, X3 AND X4 ARE EACH NO CH; C IS A COMPOUND OF FORMULA (iii), ARYL (C6-C14), AMONG OTHERS, WHERE R1 IS H, CN, HALOGEN, CF3, AMONG OTHERS; R'1, R2 AND R'2 ARE EACH H, HALOGEN, CF3, LOWER ALKYL (C1-C7), AMONG OTHERS; D IS H, HALOGEN, HYDROXYL, CN, AMONG OTHERS. PREFERRED COMPOUNDS ARE: [2- (2-CHLORO-PHENYL) -3H-BENZOIMIDAZOL-5-IL] -CARBAMIC ACID ETHYL-ESTER [2- (4-METHOXY-2-METHYL-PHENYL) ACID ETHYL-ESTER -3H-BENZOIMIDAZOLE-5-IL] -CARBAMIC, ETHYL-ESTER OF ACID [2- (2,6-DIMETHYL-PHENYL) -3H-BENZOIMIDAZOL-5-IL] -CARBAMIC, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. SUCH COMPOUNDS ARE INHIBITORS OF ACIL-COA-DIACIL-GLICEROL 1 (DGAT1) ACIL-TRANSFERASE, BEING USEFUL IN THE TREATMENT OF DETERIORATED GLUCOSE TOLERANCE, TYPE 2 DIABETES, OBESITY, ANOREXIA NERVOSA

PE2007001396A 2006-10-18 2007-10-16 HETEROCYCLIC COMPOUNDS AS ACIL-TRANSFERASE INHIBITORS OF ACIL-CoA-DIACIL-GLYCEROL 1 (DGAT1) PE20080888A1 (en)

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US82998006P 2006-10-18 2006-10-18
US95234107P 2007-07-27 2007-07-27

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US (1) US8222248B2 (en)
EP (1) EP2074089B1 (en)
JP (1) JP5298022B2 (en)
KR (1) KR20090071642A (en)
AR (1) AR063311A1 (en)
AU (1) AU2007311087B2 (en)
BR (1) BRPI0718478A2 (en)
CA (1) CA2666880A1 (en)
CL (1) CL2007002974A1 (en)
ES (1) ES2440253T3 (en)
MX (1) MX2009004047A (en)
PE (1) PE20080888A1 (en)
RU (1) RU2009118489A (en)
TW (1) TW200829563A (en)
WO (1) WO2008048991A2 (en)

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